ML133 hydrochloride

SKU: orb1300632

Description

ML133 hydrochloride is a potent and selective Kir2.1 inward rectifier potassium channel inhibitor, exhibiting pH-dependent IC50 values of 1.8 µM at pH 7.4 and 290 nM at pH 8.5. It shows minimal activity on Kir4.1 and Kir7.1 and no effect on Kir1.1, making it a valuable research tool for studying Kir2.1 function in cardiac electrophysiology and neuronal excitability in vitro.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1222781-70-5
• MW: 313.82
• Purity: 99.81%
• Formula: C₁₉H₁₉NO·HCl
• SMILES: Cl.COC1=CC=C(CNCC2=CC=CC3=CC=CC=C23)C=C1
• Target: Potassium Channel
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.37 mM);DMSO:16.67 mg/mL (53.12 mM)

Bioactivity

• Target IC50:
  KIR2.1 (pH 7.4):1.8 μM|KIR2.1 (pH 8.5):290 nM
• In Vitro:
  The ratio of total concentration of extracellular ML133 versus intracellular ML133 is 1:0.13 at pH 6.5, 1:9.09 at pH 8.5. ML133 is clean against 3A4 and 2C9 (IC50 >30 μM), displays moderate inhibition of 1A2 (IC50 = 3.3 μM) but proves to be a potent inhibitor of 2D6 (IC50 = 0.13 μM) in CYP450 assay. ML133 is highly protein bound (>99%) in both human and rat and also displays high intrinsic clearance in both species. ML133 (10 μM) is not displaced by K+ influx from the wild-type Kir2.1 in HEK 293 cells. M1 and/or M2 transmembrane domains contain the critical molecular determinant for ML133 inhibition of Kir2.1, especially D172 and I176.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Potassium Channel, PotassiumChannel, Inhibitor, KcsA, inhibit, Kir2.1, ML 133, ML 133 Hydrochloride, ML133, ML-133, ML133 HCl, ML133 hydrochloride, ML133 Hydrochloride, ML-133 Hydrochloride, ML-133 hydrochloride

Compound Identifiers

PubChem CID

44247466